TAK-779 是一种非肽类CCR5和CXCR3 拮抗剂,对CCR5的Ki值为 1.1 nM,并选择性抑制R5 HIV-1。
产品描述
TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
体外活性
TAK-779 (250 mg/animal per day) inhibits ovalbumin-induced increases in CCR5, CXCR3, IFN-γ, and TNF-α expression in mouse lung, as well as the number of total cells, lymphocytes, and eosinophils in bronchoalveolar lavage fluid (BALF), in a mouse model of asthma[1].
体内活性
TAK-779 increases intestinal allograft survival in a rat model of small intestine transplantation when administered at a dose of 10 mg/kg per day[2].
Cas No.
229005-80-5
分子式
C33H39ClN2O2
分子量
531.14
别名
Takeda 779
储存和溶解度
H2O:16.66 mg/mL (31.37 mM)
DMSO:25 mg/mL (47.07 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years